-药物合成数据库

【药物名称】

化学结构式(Chemical Structure):

参考文献No.	28083
标题:	N-Heterocyclyl sulphonamide derivs. and their use as endothelin antagonists
作者:	Bradbury, R.H. (AstraZeneca plc)
来源:	EP 0752986; JP 1997510987; US 6083951; WO 9526957

合成路线图解说明: Bromination of 2-amino-5-chloropyrazine (I) with bromine in chloroform-pyridine provided bromopyrazine (II). Then, reaction with sodium methoxide in refluxing methanol afforded methyl ether (III). Finally, condensation of (III) with dansyl chloride (IV) in the presence of NaH in dimethoxyethane yielded the corresponding sulfonamide.

参考文献No.	403302
标题:	New non-peptide endothelin-A receptor antagonists: Synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-, -N-pyrimidinyl-, -N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides
作者:	Bradbury, R.H.; Bath, C.; Butlin, R.J.; Dennis, M.; Heys, C.; Hunt, S.J.; James, R.; Mortlock, A.A.; Sumner, N.F.; Tang, E.K.; Telford, B.; Whiting, E.; Wilson, C.
来源:	J Med Chem 1997,40(6),996

合成路线图解说明: Bromination of 2-amino-5-chloropyrazine (I) with bromine in chloroform-pyridine provided bromopyrazine (II). Then, reaction with sodium methoxide in refluxing methanol afforded methyl ether (III). Finally, condensation of (III) with dansyl chloride (IV) in the presence of NaH in dimethoxyethane yielded the corresponding sulfonamide.